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A coupled chlorinase-fluorinase system with a high efficiency of trans-halogenation and a shared substrate tolerance.


ABSTRACT: Enzymatic trans-halogenation enables radiolabeling under mild and aqueous conditions, but rapid reactions are desired. We developed a coupled chlorinase-fluorinase system for rapid trans-halogenation. Notably, the chlorinase shares a substrate tolerance with the fluorinase, enabling these two enzymes to cooperatively produce 5'-fluorodeoxy-2-ethynyladenosine (5'-FDEA) in up to 91.6% yield in 1 h.

SUBMITTER: Sun H 

PROVIDER: S-EPMC6113055 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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A coupled chlorinase-fluorinase system with a high efficiency of trans-halogenation and a shared substrate tolerance.

Sun H H   Zhao H H   Ang E L EL  

Chemical communications (Cambridge, England) 20180801 68


Enzymatic trans-halogenation enables radiolabeling under mild and aqueous conditions, but rapid reactions are desired. We developed a coupled chlorinase-fluorinase system for rapid trans-halogenation. Notably, the chlorinase shares a substrate tolerance with the fluorinase, enabling these two enzymes to cooperatively produce 5'-fluorodeoxy-2-ethynyladenosine (5'-FDEA) in up to 91.6% yield in 1 h. ...[more]

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